TC-MCH 7c
目录号 : KM2783 CAS No. : 864756-35-4 纯度 : 98%

TC-MCH 7c 是一种苯基吡啶酮衍生物,一种口服有效的,选择性的且可穿透血脑屏障的 MCH1R 拮抗剂,对 hMCH1R 的 IC50 为 5.6 nM。TC-MCH 7c 对人和小鼠 MCH1R 的 Ki 分别为 3.4 nM 和 3.0 nM。

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生物活性

TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.

体外研究

TC-MCH 7c has an IC50 of 9.7 μM for MCH1R in [Ca]i mobilization.
TC-MCH 7c has IC50s of 23 nM and 9.0 μM for FLIPR and hERG, respectively.

体内研究

TC-MCH 7c (oral; 3-30 mg/kg; once-daily for 1.5 months) exhibits excellent body weight reduction in a dose-dependent manner in DIO mice model.
TC-MCH 7c (oral; 3-30 mg/kg) with 30 mg/kg has plasma concentrations of 5.1, 1.8, and 0.7 μM at 2, 15, and 24 hours, respectively.

Animal Model: C57BL/6J DIO mice
Dosage: 3, 10 and 30 mg/kg
Administration: Oral; once-daily for 1.5 months
Result: Exhibited excellent body weight reduction in a dose-dependent manner.
Animal Model: Diet-induced obesity mice
Dosage: 3, 10 and 30 mg/kg (Pharmacokinetic Analysis)
Administration: Oral
Result: Plasma concentrations at 2, 15, and 24 hours were 5.1, 1.8, and 0.7 μM, respectively.
分子式
C24H25FN2O3
分子量
408.47
CAS号
864756-35-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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